|Place of Origin:||China|
|Certification:||GMP, ISO 9001, USP|
|Model Number:||CAS 107868-30-4|
|Minimum Order Quantity:||Free samples Available|
|Packaging Details:||as your required|
|Delivery Time:||3-7 working days|
|Payment Terms:||Western Union, MoneyGram, T/T, Bitcoin|
|Supply Ability:||500-1000 kg / month|
|Melting Point:||155.13 °C||Water Solubility:||0.00683 Mg/mL|
|Appearance:||White Crystalline Powder||Biological Half-life:||24 Hours|
|Chemical Name:||6-Methylenandrosta-1,4-diene-3,17-dione||Duration Of Action:||4–5 Days|
sex hormones drugs,
natural anti estrogen
Anti Estrogen Steroids Exemestane Raw Powders for Breast Cancers
What exemestane is
Exemestane is also called Aromasin. It is a type of hormone therapy drug called an aromatase inhibitor and is used to treat breast cancer. It is only suitable for women who have had their menopause.
There is general information about hormone therapies in the cancer treatment section.
How exemestane works
Many breast cancers are stimulated to grow by the female sex hormones oestrogen and progesterone. These breast cancers are called hormone sensitive or hormone receptor positive and can be treated with drugs that block the effects of these hormones.
In women who have had their menopause, oestrogen is mainly produced by changing androgens (sex hormones produced by the adrenal glands) into oestrogens. This process is called aromatisation and happens mainly in the fatty tissues, muscle and the skin. It needs a particular enzyme called aromatase.
Exemestane blocks the process of aromatisation. So it lowers the amount of oestrogen in the body. In early breast cancer, taking exemestane can help to stop breast cancer coming back. In advanced breast cancer the cancer cells may grow more slowly or stop growing completely.
Use in Cancer
Exemestane is approved to treat:
Breast cancer that is advanced.
Breast cancer that is early-stage and estrogen receptor positive.
Exemestane is used in postmenopausal women who have already been treated with tamoxifen citrate.
Exemestane is also being studied in the treatment of other types of cancer.
Mechanism of action
Breast cancer cell growth may be estrogen-dependent. Aromatase (exemestane) is the principal enzyme that converts androgens to estrogens both in pre- and postmenopausal women. While the main source of estrogen (primarily estradiol) is the ovary in premenopausal women, the principal source of circulating estrogens in postmenopausal women is from conversion of adrenal and ovarian androgens (androstenedione and testosterone) to estrogens (estrone and estradiol) by the aromatase enzyme in peripheral tissues.
Estrogen deprivation through aromatase inhibition is an effective and selective treatment for some postmenopausal patients with hormone-dependent breast cancer. Exemestane is an irreversible, steroidal aromatase inactivator, structurally related to the natural substrate androstenedione. It acts as a false substrate for the aromatase enzyme, and is processed to an intermediate that binds irreversibly to the active site of the enzyme causing its inactivation, an effect also known as "suicide inhibition".
Exemestane significantly lowers circulating estrogen concentrations in postmenopausal women, but has no detectable effect on the adrenal biosynthesis of corticosteroids or aldosterone. This reduction in serum and tumor concentrations of estrogen delays tumor growth and disease progression. Exemestane has no effect on other enzymes involved in the steroidogenic pathway up to a concentration at least 600 times higher than that inhibiting the aromatase enzyme.
|melting point||155.13 °C||Not Available|
|Water Solubility||0.00683 mg/mL||ALOGPS|
|pKa (Strongest Acidic)||19.96||ChemAxon|
|pKa (Strongest Basic)||-5||ChemAxon|
|Hydrogen Acceptor Count||2||ChemAxon|
|Hydrogen Donor Count||0||ChemAxon|
|Polar Surface Area||34.14 Å2||ChemAxon|
|Rotatable Bond Count||0||ChemAxon|
|Number of Rings||4||ChemAxon|
|Rule of Five||Yes||ChemAxon|
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